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Assay Detail

CHEMBL4684522

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Binding
Inhibition of recombinant human PRMT8 using histone H4 as substrate by hotspot assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein arginine N-methyltransferase 3 (CHEMBL5891)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification of DOT1L inhibitors by structure-based virtual screening adapted from a nucleoside-focused library.
Gibbons GS,Chakraborty A,Grigsby SM,Umeano AC,Liao C,Moukha-Chafiq O,Pathak V,Mathew B,Lee YT,Dou Y,Schürer SC,Reynolds RC,Snowden TS,Nikolovska-Coleska Z
Eur J Med Chem (2020) 189 : 112023 -112023
PubMed 31978781 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 5.08 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL418052 S-ADENOSYLHOMOCYSTEINE 1 6.96
CHEMBL4757320 1 4.27
CHEMBL4755253 1 4.02
CHEMBL4787257 1 -
CHEMBL4777038 1 -
CHEMBL4740900 1 -
CHEMBL4765125 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL418052 S-ADENOSYLHOMOCYSTEINE IC50 = 110.0 nM 6.96
CHEMBL4757320 IC50 = 53600.0 nM 4.27
CHEMBL4755253 IC50 = 94900.0 nM 4.02
CHEMBL4787257 IC50 = 216000.0 nM -
CHEMBL4777038 IC50 - -
CHEMBL4740900 IC50 - -
CHEMBL4765125 IC50 > 250000.0 nM -